Vocacapsaicin, formerly designated as CA-008 HCl, is a novel prodrug of trans-capsaicin (trans-8-methyl-N-vanillyl-6-nonenamide) being developed as a nonopioid, site-specific treatment for postsurgical pain management. It is designed to provide long-lasting (at least 96?h) postsurgical analgesia following a single intraoperative administration. The free base form of vocacapsaicin rapidly cyclizes under physiological conditions to yield active capsaicin and CA-101 (cyclic urea) as the sole conversion products. Vocacapsaicin was developed to improve the solubility profile of capsaicin and allow for an aqueous formulation that could be simply administered at the wound site to achieve a long-lasting analgesic effect. Vocacapsaicin has little or no pharmacologic activity as the intact prodrug and is rapidly converted to capsaicin[1].
생물학적 활성
Vocacapsaicin (CA-008) hydrochloride, a proagent of Capsaicin, is a first-in-class non-opioid TRPV1 agonist. Vocacapsaicin hydrochloride can provide meaningful and long-lasting pain relief.
Mechanism of action
Vocacapsaicin is an innovative water-soluble prodrug that rapidly releases capsaicin. The design of this prodrug aims to activate TRPV1 receptors through topical administration. Capsaicin can induce a long-term non-responsive state in C-fibers, providing a sustained analgesic effect without affecting sensation, proprioception, or muscle strength.
